2. Epigenetics
  3. TET Protein
  4. TETi76

TETi76 is an orally active TET family inhibitor with IC50 values of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.

For research use only. We do not sell to patients.

TETi76 Chemical Structure

TETi76 Chemical Structure

CAS No. : 1451750-73-4

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

TETi76 Related Antibodies

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TET1 TET2 TET3

  • Biological Activity

  • Purity & Documentation

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Description

TETi76 is an orally active TET family inhibitor with IC50 values of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research[1].

IC50 & Target[1]

TET1

1.5 μM (IC50)

TET2

9.4 μM (IC50)

TET3

8.8 μM (IC50)

In Vitro

TETi76 (25 μM; 3 d) induces cell death and inhibits TET dioxygenase activity in SIG-M5 cells[1]. TETi76 (20-37 μM; 12 h) reduces intracellular 5 hmC content in a dose-dependent manner in various human leukemia cell lines (K562, MEG-01, SIG-M5, OCI-AML5, and MOLM13), with the concentration range of 50% inhibition of 5 hmC being 20-37 μM[1].
TETi76 (25 μM; 24 h) mimicks the expression signature caused by TET2 deficiency in gene expression analysis of K562 (TET2 (+/+) and TET2 (-/-) cells, and addition of ascorbic acid, known to enhance TET activity, counteracts the changes induced by TETi76[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TETi76 Related Antibodies
In Vivo

TETi76 (50 mg/kg; oral; 5 days per week; 3 months) has no significant effect on the total body weight and overall blood cell counts of mice in Tet2+/+, Tet2+/-, and Tet2-/- mouse models on the C57BL6 background, but reduces the spleen size of Tet2-deficient mice in a gene dose-dependent manner[1].
TETi76 (25 mg/kg; ip; once daily, 5 days per week; 4 weeks) limits the proliferative advantage of Tet2 / (CD45.2) cells in the C57BL6 CD45.1 Pep Boy mouse model (lethally irradiated and transplanted with mixed bone marrow cells) without affecting the proportion of mice receiving Tet2+/+ (CD45.2) cells[1].
TETi76 (50 mg/kg; oral) significantly reduces tumor burden in the immunodeficient NSG mouse model (subcutaneously implanted with the human TET2 / leukemia cell line SIG-M5)[1]).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL6 mice (sex not specified, weight not specified, age not specified) with Tet2+/+, Tet2+/− and Tet2−/− genotypes + Mouse model for observing the effect of TETi76 on spleen size and general health[1]
Dosage: 50 mg/kg
Administration: Oral administration, 5 days per week, for 3 months
Result: Did not show significant changes in the overall body weight and overall blood counts of the mice compared with the placebo group.
Decreased the spleen sizes of Tet2-deficient mice in a gene dose-dependent manner.
Molecular Weight

216.23

Formula

C10H16O5
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

O=C(OCC)C(O)CC(C(OCC)=O)=C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (462.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6247 mL 23.1235 mL 46.2471 mL
5 mM 0.9249 mL 4.6247 mL 9.2494 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (11.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (11.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 97.49%

SDS (393 KB)

COA (243 KB) HNMR (201 KB) LCMS (146 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.6247 mL 23.1235 mL 46.2471 mL 115.6176 mL
5 mM 0.9249 mL 4.6247 mL 9.2494 mL 23.1235 mL
10 mM 0.4625 mL 2.3124 mL 4.6247 mL 11.5618 mL
15 mM 0.3083 mL 1.5416 mL 3.0831 mL 7.7078 mL
20 mM 0.2312 mL 1.1562 mL 2.3124 mL 5.7809 mL
25 mM 0.1850 mL 0.9249 mL 1.8499 mL 4.6247 mL
30 mM 0.1542 mL 0.7708 mL 1.5416 mL 3.8539 mL
40 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8904 mL
50 mM 0.0925 mL 0.4625 mL 0.9249 mL 2.3124 mL
60 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9270 mL
80 mM 0.0578 mL 0.2890 mL 0.5781 mL 1.4452 mL
100 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
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TETi76 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TETi761451750-73-4TETi 76TETi-76TET ProteinTET enzymeTen-eleven-translocation (TET) proteinTen-eleven translocation (TET) methylcytosine dioxygenaseCompetitive inhibitionactive sitehydroxymethylationleukemiaInhibitorinhibitorinhibit

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